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187735-94-0

中文名稱 化合物BIO-1211
英文名稱 BIO 1211
CAS 187735-94-0
分子式 C36H48N6O9
分子量 708.8
MOL 文件 187735-94-0.mol
更新日期 2023/03/20 15:41:17
187735-94-0 結(jié)構(gòu)式 187735-94-0 結(jié)構(gòu)式

基本信息

中文別名
化合物BIO-1211
(2S)-1-[(2S)-2-[[(2S)-3-CARBOXY-2-[[(2S)-4-METHYL-2-[[2-[4-[(2-METHYLPHENYL)CARBAMOYLAMINO]PHENYL]ACETYL]AMINO]PENTANOYL]AMINO]PROPANOYL]AMINO]-3-METHYLBUTANOYL]PYRROLIDINE-2-CARBOXYLIC ACID
英文別名
BIO 1211
inhibit,BIO1211,BIO-1211,Integrin,BIO 1211,Inhibitor
L-Proline, N-[2-[4-[[[(2-methylphenyl)amino]carbonyl]amino]phenyl]acetyl]-L-leucyl-L-α-aspartyl-L-valyl-
(2S)-1-[(2S)-2-[[(2S)-3-carboxy-2-[[(2S)-4-methyl-2-[[2-[4-[(2-methylphenyl)carbamoylamino]phenyl]acetyl]amino]pentanoyl]amino]propanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carboxylicacid

物理化學(xué)性質(zhì)

沸點(diǎn)962.2±65.0 °C(Predicted)
密度1.306±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度Soluble to 2 mg/ml in 0.2M PBS
酸度系數(shù)(pKa)3.40±0.20(Predicted)
形態(tài)固體
顏色白色
水溶解性Soluble to 2 mg/ml in water
化合物BIO-1211價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2025/02/08HY-14126化合物BIO-1211
BIO-1211
187735-94-01mg1400元
2025/02/08HY-14126化合物BIO-1211
BIO-1211
187735-94-05 mg3500元
2025/02/08HY-14126化合物BIO-1211
BIO-1211
187735-94-010 mg5450元

常見問(wèn)題列表

生物活性
BIO-1211 是高度選擇性的、具有口服活性的 α4β1 (VLA-4) 抑制劑,其對(duì) α4β1 和 α4β7 的 IC50 值分別為 4 nM 和 2 μM。
靶點(diǎn)

α4β1

4 nM (IC 50 )

α4β7

2 μM (IC 50 )

α1β1

>100 μM (IC 50 )

α5β1

>100 μM (IC 50 )

α6β1

>100 μM (IC 50 )

αLβ2

>100 μM (IC 50 )

αIIbβ3

>100 μM (IC 50 )

體內(nèi)研究

BIO-1211 (5 and 10 mg/kg, orally, once every other day) results in reduced cytokines expression, leukocyte trafficking, and inhibition of inflammatory responses in EAE in a dose-independent manner. BIO-1211 exhibits a considerable depletion in the EAE clinical score, which correlated with decreased expression of TNF-α, IL-17, IFN-γ and pervade of CD11b+ and CD45+ cells into the cerebral cortex.

Animal Model: Naive, C57BL/6 mice (male, 8 weeks old, 20-25 g weight).
Dosage: 5 and 10 mg/kg.
Administration: Orally once every other day starting the day before immunization until day 21 post-immunization.
Result: Could prevent the induction of EAE.
Significantly delayed the onset of EAE and reduced the severity of clinical EAE compared to the vehicle group.
Markedly reduced the expression of both CD11b and CD45 in comparison with the vehicle group.
mRNA and soluble form of a subset of target inflammatory cytokines (IFNγ, IL-17, and TNF-α) was dramatically decreased.
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